General Information of the Protein
Protein ID
PT01683
Protein Name
Arachidonate 5-lipoxygenase-activating protein
Secondarily
Protein Name
FLAP
MK-886-binding protein
Gene Name
ALOX5AP
Secondarily
Gene Name
FLAP
Sequence
MDQETVGNVVLLAIVTLISVVQNGFFAHKVEHESRTQNGRSFQRTGTLAFERVYTANQNCVDAYPTFLAVLWSAGLLCSQVPAAFAGLMYLFVRQKYFVGYLGERTQSTPGYIFGKRIILFLFLMSVAGIFNYYLIFFFGSDFENYIKTISTTISPLLLIP
    Show/Hide
Organism
Homo sapiens, Human
Protein Classification
Other cytosolic protein
Function
Required for leukotriene biosynthesis by ALOX5 (5-lipoxygenase). Anchors ALOX5 to the membrane. Binds arachidonic acid, and could play an essential role in the transfer of arachidonic acid to ALOX5. Binds to MK-886, a compound that blocks the biosynthesis of leukotrienes.
    Show/Hide
Uniprot ID
Primary ID:
P20292

Secondarily ID:
Q5VV04
    Show/Hide
Ensembl ID
ENSG00000132965
HGNC ID
HGNC:436
Subcellular Location
Nucleus membrane
Endoplasmic reticulum membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000053 , COS-7
Compound ID Compound Name Compound Formula
CP0098465
2-methyl-N-[(2-methylpropan-2-yl)oxy]-4-[[(1R,2R)-2-[4-(5-methyl-1H-pyrazol-3-yl)benzoyl]cyclohexanecarbonyl]amino]pyrazole-3-carboxamide
   Show/Hide
C27H34N6O4
 1
1
IC50 = 5.8 nM
   TI
   LI
   LO
   TS
CP0063832
(1R,2R)-2-[4-(5-methyl-1H-pyrazol-3-yl)benzoyl]-N-(4-oxo-6,7-dihydro-5H-pyrazolo[1,5-a]pyrazin-3-yl)cyclohexane-1-carboxamide
   Show/Hide
C24H26N6O3
 1
1
IC50 = 6.3 nM
   TI
   LI
   LO
   TS
CP0534508
(1R,2R)-N-[3-(difluoromethyl)-1-methylpyrazol-4-yl]-2-[4-(5-methyl-1H-pyrazol-3-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C23H25F2N5O2
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0356625
(1S,3R,4R,6R)-N-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]-4-[4-(1H-pyrazol-5-yl)benzoyl]bicyclo[4.1.0]heptane-3-carboxamide
   Show/Hide
C23H22F3N5O2
 1
1
IC50 = 12.59 nM
   TI
   LI
   LO
   TS
CP0534510
(1S,3R,4R,6R)-N-[1-methyl-5-(trifluoromethyl)pyrazol-4-yl]-4-[4-(1H-pyrazol-5-yl)benzoyl]bicyclo[4.1.0]heptane-3-carboxamide
   Show/Hide
C23H22F3N5O2
 1
1
IC50 = 12.59 nM
   TI
   LI
   LO
   TS
CP0149564
(1R,2R)-N-(6-methoxypyrimidin-4-yl)-2-[4-(1H-pyrazol-5-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C22H23N5O3
 1
1
IC50 = 15.85 nM
   TI
   LI
   LO
   TS
CP0238638
N-(2-hydroxy-2-methylpropyl)-5-[[(1R,2R)-2-[4-(1H-pyrazol-5-yl)benzoyl]cyclohexanecarbonyl]amino]pyrazine-2-carboxamide
   Show/Hide
C26H30N6O4
 1
1
IC50 = 15.85 nM
   TI
   LI
   LO
   TS
CP0426861
2-methyl-4-[[(1R,2R)-2-[4-(5-methyl-1H-pyrazol-3-yl)benzoyl]cyclohexanecarbonyl]amino]pyrazole-3-carboxylic acid
   Show/Hide
C23H25N5O4
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0476659
(1R,2R)-N-(3-cyano-1-methylpyrazol-4-yl)-2-[4-(5-methyl-1H-pyrazol-3-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C23H24N6O2
 1
1
IC50 = 19.95 nM
   TI
   LI
   LO
   TS
CP0564783
5-methyl-4-[[(1R,2R)-2-[4-(5-methyl-1H-pyrazol-3-yl)benzoyl]cyclohexanecarbonyl]amino]-1H-pyrazole-3-carboxamide
   Show/Hide
C23H26N6O3
 1
1
IC50 = 24 nM
   TI
   LI
   LO
   TS
CP0139650
(1R,2R)-N-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]-2-[4-(1H-pyrazol-5-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C22H22F3N5O2
 1
1
IC50 = 25.12 nM
   TI
   LI
   LO
   TS
CP0960908
1-ethyl-4-((1R,2R)-2-(4-(3-methyl-1H-pyrazol-5-yl)benzoyl)cyclohexanecarboxamido)-1H-pyrazole-5-carboxamide
   Show/Hide
C24H28N6O3
 1
1
IC50 = 29 nM
   TI
   LI
   LO
   TS
CP0238652
(1R,2R)-N-pyrazolo[1,5-a]pyrimidin-3-yl-2-[4-(1H-pyrazol-5-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C23H22N6O2
 1
1
IC50 = 31.62 nM
   TI
   LI
   LO
   TS
CP0534697
(1R,2R)-N-[3-(difluoromethoxy)-1-methylpyrazol-4-yl]-2-[4-(1H-pyrazol-5-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C22H23F2N5O3
 1
1
IC50 = 31.62 nM
   TI
   LI
   LO
   TS
CP0098466
(1R,2R)-2-[4-(5-methyl-1H-pyrazol-3-yl)benzoyl]-N-(1-methyl-5-sulfamoylpyrazol-4-yl)cyclohexane-1-carboxamide
   Show/Hide
C22H26N6O4S
 1
1
IC50 = 34 nM
   TI
   LI
   LO
   TS
CP0959472
1-methyl-4-((1R,2R)-2-(4-(3-methyl-1H-pyrazol-5-yl)benzoyl)cyclohexanecarboxamido)-1H-pyrazole-5-carboxamide
   Show/Hide
C23H26N6O3
 1
1
IC50 = 35 nM
   TI
   LI
   LO
   TS
CP0149566
1-methyl-4-[[(1R,2R)-2-[4-(5-methyl-1H-pyrazol-3-yl)benzoyl]cyclohexanecarbonyl]amino]pyrazole-3-carboxamide
   Show/Hide
C23H26N6O3
 2
1
IC50 = 36 nM
   TI
   LI
   LO
   TS
2
IC50 = 39.81 nM
   TI
   LI
   LO
   TS
CP0347329
1-methyl-4-[[(1S,3R,4R,6R)-4-[6-(5-methyl-1H-pyrazol-3-yl)-1,2-benzoxazol-3-yl]bicyclo[4.1.0]heptane-3-carbonyl]amino]pyrazole-3-carboxamide
   Show/Hide
C24H25N7O3
 1
1
IC50 = 39.81 nM
   TI
   LI
   LO
   TS
CP0532531
(1R,2R)-N-[1-methyl-5-(trifluoromethyl)pyrazol-4-yl]-2-[4-(1H-pyrazol-5-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C22H22F3N5O2
 1
1
IC50 = 39.81 nM
   TI
   LI
   LO
   TS
CP0575284
N-hydroxy-2-methyl-4-[[(1R,2R)-2-[4-(5-methyl-1H-pyrazol-3-yl)benzoyl]cyclohexanecarbonyl]amino]pyrazole-3-carboxamide
   Show/Hide
C23H26N6O4
 1
1
IC50 = 47 nM
   TI
   LI
   LO
   TS
CP0028152
(1R,2R)-N-(1,3-dimethylpyrazol-4-yl)-2-[4-(5-methyl-1H-pyrazol-3-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C23H27N5O2
 2
1
IC50 = 59 nM
   TI
   LI
   LO
   TS
2
IC50 = 63.1 nM
   TI
   LI
   LO
   TS
CP0493797
(2R,3R)-N-(1,3-dimethylpyrazol-4-yl)-3-[2-fluoro-4-(1H-pyrazol-5-yl)benzoyl]bicyclo[2.2.2]octane-2-carboxamide
   Show/Hide
C24H26FN5O2
 1
1
IC50 = 63.1 nM
   TI
   LI
   LO
   TS
CP0534414
(1R,2R)-N-(2-methyl-2-methylsulfonylpropyl)-2-[4-(1H-pyrazol-5-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C22H29N3O4S
 1
1
IC50 = 63.1 nM
   TI
   LI
   LO
   TS
CP0238653
1-methyl-4-[[(1R,2R)-2-[6-(5-methyl-1H-pyrazol-3-yl)-1,2-benzoxazol-3-yl]cyclohexanecarbonyl]amino]pyrazole-3-carboxamide
   Show/Hide
C23H25N7O3
 1
1
IC50 = 79.43 nM
   TI
   LI
   LO
   TS
CP0356624
4-[[(1R,2R)-2-[2-fluoro-4-(5-methyl-1H-pyrazol-3-yl)benzoyl]cyclohexanecarbonyl]amino]-1-methylpyrazole-3-carboxamide
   Show/Hide
C23H25FN6O3
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0564782
2,5-dimethyl-4-[[(1R,2R)-2-[4-(5-methyl-1H-pyrazol-3-yl)benzoyl]cyclohexanecarbonyl]amino]pyrazole-3-carboxamide
   Show/Hide
C24H28N6O3
 1
1
IC50 = 101 nM
   TI
   LI
   LO
   TS
CP0476658
(1R,2R)-N-(1,3-dimethylpyrazol-4-yl)-2-[2-fluoro-4-(1H-pyrazol-5-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C22H24FN5O2
 1
1
IC50 = 125.89 nM
   TI
   LI
   LO
   TS
CP0476660
(1R,2R)-N-(3,5-dimethyl-1,2-oxazol-4-yl)-2-[4-(1H-pyrazol-5-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C22H24N4O3
 1
1
IC50 = 199.53 nM
   TI
   LI
   LO
   TS
CP0517700
(1R,2R)-N-(1,3-dimethylpyrazol-4-yl)-N-methyl-2-[4-(1H-pyrazol-5-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C23H27N5O2
 1
1
IC50 = 199.53 nM
   TI
   LI
   LO
   TS
CP0569617
(1R,2R)-N-[1-(2-amino-2-oxoethyl)pyrazol-4-yl]-2-[4-(5-methyl-1H-pyrazol-3-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C23H26N6O3
 1
1
IC50 = 241 nM
   TI
   LI
   LO
   TS
CP0482640
(1R,2R)-2-[4-(1H-pyrazol-5-yl)benzoyl]-N-(2-pyridin-2-ylethyl)cyclohexane-1-carboxamide
   Show/Hide
C24H26N4O2
 1
1
IC50 = 251.19 nM
   TI
   LI
   LO
   TS
CP0534415
3-[[(1R,2R)-2-[4-(4-methylpyrazol-1-yl)benzoyl]cyclohexanecarbonyl]amino]benzamide
   Show/Hide
C25H26N4O3
 1
1
IC50 = 316.23 nM
   TI
   LI
   LO
   TS
CP0532530
(1R,2R)-N-(1,3-dimethylpyrazol-4-yl)-2-(4-pyridin-2-ylbenzoyl)cyclohexane-1-carboxamide
   Show/Hide
C24H26N4O2
 1
1
IC50 = 501.19 nM
   TI
   LI
   LO
   TS
CP0438857
(1R,2R)-N-(1,3-dimethylpyrazol-4-yl)-2-[4-(4-methyl-1H-pyrazol-5-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C23H27N5O2
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0517701
(1R,2R)-N-(1,3-dimethylpyrazol-4-yl)-2-[4-(1H-pyrrol-2-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C23H26N4O2
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0570263
(1R,2R)-N-(1,3-dimethylpyrazol-4-yl)-2-[6-(1H-pyrazol-5-yl)pyridine-3-carbonyl]cyclohexane-1-carboxamide
   Show/Hide
C21H24N6O2
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0574082
(1R,2R)-N-(1,3-dimethylpyrazol-4-yl)-2-[2-methyl-4-(1H-pyrazol-5-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C23H27N5O2
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0529545
(1S,2S)-N-(1,3-dimethylpyrazol-4-yl)-2-[4-(1H-pyrazol-5-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C22H25N5O2
 1
1
IC50 = 1995.26 nM
   TI
   LI
   LO
   TS
CP0441041
(1R,2R)-2-[4-(3-acetylphenyl)benzoyl]-N-(3,5-dimethyl-1,2-oxazol-4-yl)cyclohexane-1-carboxamide
   Show/Hide
C27H28N2O4
 1
1
IC50 = 2511.89 nM
   TI
   LI
   LO
   TS
CP0441040
(1R,2R)-N-(1,3-dimethylpyrazol-4-yl)-2-[4-(2-methylpyrazol-3-yl)benzoyl]cyclohexane-1-carboxamide
   Show/Hide
C23H27N5O2
 1
1
IC50 = 25118.86 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0029907
2-[4-[3-[(1R)-1-[4-(2-aminopyrimidin-5-yl)phenyl]-1-cyclopropylethyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]-N,N-dimethylacetamide
   Show/Hide
C24H26N8O2
 3
1 IC50 = 1.7 nM
2 IC50 = 45 nM
3 IC50 ~ 1.7 nM
CP0086097
US8575201, 80
   Show/Hide
C19H18N8O
 2
1 IC50 = 5.5 nM
2 IC50 = 164 nM
CP0129226
US8575201, 63
   Show/Hide
C20H20N8O
 2
1 IC50 = 8.8 nM
2 IC50 = 192 nM
CP0315670
5-[5-[(1R)-1-cyclopropyl-1-[5-[1-(oxetan-3-yl)pyrazol-4-yl]-1,2,4-oxadiazol-3-yl]ethyl]pyridin-2-yl]pyrimidin-2-amine
   Show/Hide
C22H22N8O2
 1
1 IC50 = 12 nM
CP0110933
US8575201, 55
   Show/Hide
C21H20N8O2
 2
1 IC50 = 13 nM
2 IC50 = 71 nM
CP0271141
US8575201, 102
   Show/Hide
C19H18N8O
 2
1 IC50 = 13 nM
2 IC50 = 270 nM
CP0548820
1-[3-[(1R)-1-[4-(2-aminopyrimidin-5-yl)phenyl]-1-cyclopropylethyl]-1,2,4-oxadiazol-5-yl]-4-methylpiperidin-4-ol
   Show/Hide
C23H28N6O2
 1
1 IC50 = 13 nM
CP0183149
5-[4-[(1R)-1-cyclopropyl-1-[5-[1-[2-(dimethylamino)ethyl]pyrazol-4-yl]-1,2,4-oxadiazol-3-yl]ethyl]phenyl]pyrimidin-2-amine
   Show/Hide
C24H28N8O
 1
1 IC50 = 14 nM
CP0175132
US8575201, 144
   Show/Hide
C24H27N9O2
 2
1 IC50 = 14 nM
2 IC50 = 195 nM
CP0175191
US8575201, 143
   Show/Hide
C25H29N9O2
 2
1 IC50 = 14 nM
2 IC50 = 262 nM
CP0326561
5-[4-[(1R)-1-cyclopropyl-1-[5-(1-methylpyrazol-4-yl)-1,2,4-oxadiazol-3-yl]ethyl]phenyl]pyrimidin-2-amine
   Show/Hide
C21H21N7O
 1
1 IC50 = 15 nM
CP0343152
US8575201, 28
   Show/Hide
C21H22N8O2
 2
1 IC50 = 17 nM
2 IC50 = 213 nM
CP0179823
US8575201, 151
   Show/Hide
C22H21N9O
 2
1 IC50 = 18 nM
2 IC50 = 94 nM
CP0127452
2-[4-[3-[(1R)-1-[6-(2-aminopyrimidin-5-yl)pyridin-3-yl]-1-cyclopropylethyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]acetonitrile
   Show/Hide
C21H19N9O
 1
1 IC50 = 19 nM
CP0199283
1-[4-[3-[(1R)-1-[4-(2-aminopyrimidin-5-yl)phenyl]-1-cyclopropylethyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]-2-methylpropan-2-ol
   Show/Hide
C24H27N7O2
 1
1 IC50 = 20 nM
CP0261517
1-[3-[(2R)-2-[4-(2-aminopyrimidin-5-yl)phenyl]-3-methylbutan-2-yl]-1,2,4-oxadiazol-5-yl]-4-methylpiperidin-4-ol
   Show/Hide
C23H30N6O2
 1
1 IC50 = 21 nM
CP0370073
5-[5-[(1R)-1-cyclopropyl-1-[5-(1-methylpyrazol-4-yl)-1,2,4-oxadiazol-3-yl]ethyl]pyridin-2-yl]pyrimidin-2-amine
   Show/Hide
C20H20N8O
 1
1 IC50 = 26 nM
CP0475862
2-[4-[3-[1-[4-(2-aminopyrimidin-5-yl)phenyl]cyclobutyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]-N-tert-butyl-N-methylacetamide
   Show/Hide
C26H30N8O2
 1
1 IC50 = 27 nM
CP0237377
US8575201, 54
   Show/Hide
C22H24N8O2
 2
1 IC50 = 28 nM
2 IC50 = 124 nM
CP0499953
2-[4-[3-[(1R)-1-cyclopropyl-1-[4-[2-(methylamino)pyrimidin-5-yl]phenyl]ethyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]-N,N-dimethylacetamide
   Show/Hide
C25H28N8O2
 1
1 IC50 = 30 nM
CP0302589
5-[4-[(2R)-3-methyl-2-[5-(1-methylpyrazol-4-yl)-1,2,4-oxadiazol-3-yl]butan-2-yl]phenyl]pyrimidin-2-amine
   Show/Hide
C21H23N7O
 1
1 IC50 = 33 nM
CP0175129
US8575201, 30
   Show/Hide
C22H24N8O2
 2
1 IC50 = 33 nM
2 IC50 = 403 nM
CP0370074
5-[5-[(2R)-3-methyl-2-[5-(1-methylpyrazol-4-yl)-1,2,4-oxadiazol-3-yl]butan-2-yl]pyridin-2-yl]pyrimidin-2-amine
   Show/Hide
C20H22N8O
 1
1 IC50 = 33 nM
CP0237378
1-[3-[(1R)-1-[4-(2-aminopyrimidin-5-yl)phenyl]-1-cyclopropylethyl]-1,2,4-oxadiazol-5-yl]piperidin-4-ol
   Show/Hide
C22H26N6O2
 1
1 IC50 = 37 nM
CP0239441
5-[5-[(2R)-3-methyl-2-[5-[1-(oxetan-3-yl)pyrazol-4-yl]-1,2,4-oxadiazol-3-yl]butan-2-yl]pyridin-2-yl]pyrimidin-2-amine
   Show/Hide
C22H24N8O2
 1
1 IC50 = 37 nM
CP0417387
3-[4-[3-[1-[4-(2-aminopyrimidin-5-yl)phenyl]cyclobutyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]propanenitrile
   Show/Hide
C22H20N8O
 1
1 IC50 = 37 nM
CP0127411
2-[4-[3-[1-[4-(2-aminopyrimidin-5-yl)phenyl]cyclobutyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]-N-tert-butylacetamide
   Show/Hide
C25H28N8O2
 1
1 IC50 = 40 nM
CP0315671
2-[4-[3-[(2R)-2-[6-(2-aminopyrimidin-5-yl)pyridin-3-yl]-3-methylbutan-2-yl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]acetonitrile
   Show/Hide
C21H21N9O
 1
1 IC50 = 40 nM
CP0370075
1-[4-[3-[(1R)-1-[6-(2-aminopyrimidin-5-yl)pyridin-3-yl]-1-cyclopropylethyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]-2-methylpropan-2-ol
   Show/Hide
C23H26N8O2
 1
1 IC50 = 41 nM
CP0541241
1-[4-[3-[(2R)-2-[6-(2-aminopyrimidin-5-yl)pyridin-3-yl]-3-methylbutan-2-yl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]-2-methylpropan-2-ol
   Show/Hide
C23H28N8O2
 1
1 IC50 = 41 nM
CP0237376
US8575201, 133
   Show/Hide
C19H18N8O
 2
1 IC50 = 43 nM
2 IC50 = 342 nM
CP0271149
5-[4-[1-[5-[1-(oxetan-3-yl)pyrazol-4-yl]-1,2,4-oxadiazol-3-yl]cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C22H21N7O2
 1
1 IC50 = 43 nM
CP0369521
5-[4-[1-[5-(1-methylpyrazol-4-yl)-1,2,4-oxadiazol-3-yl]cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C20H19N7O
 1
1 IC50 = 45 nM
CP0350128
5-[4-[3-methyl-2-[5-(1-methylpyrazol-4-yl)-1,2,4-oxadiazol-3-yl]butan-2-yl]phenyl]pyrimidin-2-amine
   Show/Hide
C21H23N7O
 1
1 IC50 = 46 nM
CP0245531
5-[4-[1-[5-[1-[2-(dimethylamino)ethyl]pyrazol-4-yl]-1,2,4-oxadiazol-3-yl]cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C23H26N8O
 1
1 IC50 = 47 nM
CP0239440
2-[4-[3-[(1R)-1-[6-(2-aminopyrimidin-5-yl)pyridin-3-yl]-1-cyclopropylethyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]-N,N-dimethylacetamide
   Show/Hide
C23H25N9O2
 1
1 IC50 = 48 nM
CP0082986
1-[3-[(2R)-2-[4-(2-aminopyrimidin-5-yl)phenyl]-3-methylbutan-2-yl]-1,2,4-oxadiazol-5-yl]piperidin-4-ol
   Show/Hide
C22H28N6O2
 1
1 IC50 = 55 nM
CP0489154
4-[3-[(1R)-1-[4-(2-aminopyrimidin-5-yl)phenyl]-1-cyclopropylethyl]-1,2,4-oxadiazol-5-yl]-N,N-dimethylpiperazine-1-carboxamide
   Show/Hide
C24H30N8O2
 1
1 IC50 = 58 nM
CP0302588
5-[4-[1-[5-[1-(2-methoxyethyl)pyrazol-4-yl]-1,2,4-oxadiazol-3-yl]cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C22H23N7O2
 1
1 IC50 = 65 nM
CP0444934
2-[4-[3-[(1R)-1-[4-(6-aminopyridin-3-yl)phenyl]-1-cyclopropylethyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]-N,N-dimethylacetamide
   Show/Hide
C25H27N7O2
 1
1 IC50 = 66 nM
CP0127412
1-[4-[3-[1-[4-(2-aminopyrimidin-5-yl)phenyl]cyclobutyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]-2-methylpropan-2-ol
   Show/Hide
C23H25N7O2
 1
1 IC50 = 69 nM
CP0364379
1-[3-[(1R)-1-[4-(2-aminopyrimidin-5-yl)phenyl]-1-cyclopropylethyl]-1,2,4-oxadiazol-5-yl]-3-methylazetidin-3-ol
   Show/Hide
C21H24N6O2
 1
1 IC50 = 72 nM
CP0302590
2-[4-[3-[(1R)-1-[4-(5-aminopyrazin-2-yl)phenyl]-1-cyclopropylethyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]-N,N-dimethylacetamide
   Show/Hide
C24H26N8O2
 1
1 IC50 = 73 nM
CP0369520
5-[4-[1-[5-(5-methyl-1H-pyrazol-3-yl)-1,2,4-oxadiazol-3-yl]cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C20H19N7O
 1
1 IC50 = 80 nM
CP0324942
2-[4-[3-[1-[4-(2-aminopyrimidin-5-yl)phenyl]cyclobutyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]-N,N-dimethylacetamide
   Show/Hide
C23H24N8O2
 1
1 IC50 = 81 nM
CP0237477
US8575201, 134
   Show/Hide
C19H18N8O
 2
1 IC50 = 81 nM
2 IC50 = 787 nM
CP0408352
3-[4-[3-[1-[6-(2-aminopyrimidin-5-yl)pyridin-3-yl]cyclobutyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]propanenitrile
   Show/Hide
C21H19N9O
 1
1 IC50 = 85 nM
CP0271150
1-[3-[1-[4-(2-aminopyrimidin-5-yl)phenyl]cyclobutyl]-1,2,4-oxadiazol-5-yl]-4-methylpiperidin-4-ol
   Show/Hide
C22H26N6O2
 1
1 IC50 = 87 nM
CP0177304
5-[4-[(1R)-1-cyclobutyl-1-[5-(1-methylpyrazol-4-yl)-1,2,4-oxadiazol-3-yl]ethyl]phenyl]pyrimidin-2-amine
   Show/Hide
C22H23N7O
 1
1 IC50 = 91 nM
CP0085835
US8575201, 76
   Show/Hide
C19H21N7O
 2
1 IC50 = 92 nM
2 IC50 = 917 nM
CP0271151
3-[(1R)-1-[4-(2-aminopyrimidin-5-yl)phenyl]-1-cyclopropylethyl]-N-methyl-N-(1-methylpyrazol-4-yl)-1,2,4-oxadiazol-5-amine
   Show/Hide
C22H24N8O
 1
1 IC50 = 92 nM
CP0324943
5-[4-[2-[5-(1-methylpyrazol-4-yl)-1,2,4-oxadiazol-3-yl]propan-2-yl]phenyl]pyrimidin-2-amine
   Show/Hide
C19H19N7O
 1
1 IC50 = 93 nM
CP0127415
1-[4-[3-[(1R)-1-[4-(2-aminopyrimidin-5-yl)phenyl]-1-cyclopropylethyl]-1,2,4-oxadiazol-5-yl]piperazin-1-yl]-2-methylpropan-2-ol
   Show/Hide
C25H33N7O2
 1
1 IC50 = 99 nM
CP0316800
5-[4-[1-[5-(1H-pyrazol-4-yl)-1,2,4-oxadiazol-3-yl]cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C19H17N7O
 1
1 IC50 = 110 nM
CP0475867
1-[3-[(1R)-1-[6-(2-aminopyrimidin-5-yl)pyridin-3-yl]-1-cyclopropylethyl]-1,2,4-oxadiazol-5-yl]-4-methylpiperidin-4-ol
   Show/Hide
C22H27N7O2
 1
1 IC50 = 115 nM
CP0082984
1-[3-[1-[4-(2-aminopyrimidin-5-yl)phenyl]cyclobutyl]-1,2,4-oxadiazol-5-yl]piperidin-4-ol
   Show/Hide
C21H24N6O2
 1
1 IC50 = 118 nM
CP0541502
2-[4-[3-[1-[4-(2-aminopyrimidin-5-yl)phenyl]cyclobutyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]-2-methylpropan-1-ol
   Show/Hide
C23H25N7O2
 1
1 IC50 = 155 nM
CP0238791
5-[4-[1-[5-(1H-pyrazol-5-yl)-1,2,4-oxadiazol-3-yl]cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C19H17N7O
 1
1 IC50 = 160 nM
CP0110937
US8575201, 154
   Show/Hide
C20H23N7O2
 2
1 IC50 = 170 nM
2 IC50 = 595 nM
CP0370071
[1-[3-[1-[4-(2-aminopyrimidin-5-yl)phenyl]cyclobutyl]-1,2,4-oxadiazol-5-yl]piperidin-4-yl]methanol
   Show/Hide
C22H26N6O2
 1
1 IC50 = 173 nM
CP0463371
5-[4-[1-[5-(4-propan-2-yloxypiperidin-1-yl)-1,2,4-oxadiazol-3-yl]cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C24H30N6O2
 1
1 IC50 = 174 nM
CP0389228
5-[4-[1-[5-[4-(oxolan-2-ylmethyl)piperazin-1-yl]-1,2,4-oxadiazol-3-yl]cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C25H31N7O2
 1
1 IC50 = 182 nM
CP0177302
5-[4-[2-methyl-1-[5-(1-methylpyrazol-4-yl)-1,2,4-oxadiazol-3-yl]propyl]phenyl]pyrimidin-2-amine
   Show/Hide
C20H21N7O
 1
1 IC50 = 190 nM
CP0083001
2-[4-[3-[(2R)-2-[6-(2-aminopyrimidin-5-yl)pyridin-3-yl]-3-methylbutan-2-yl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]-N,N-dimethylacetamide
   Show/Hide
C23H27N9O2
 1
1 IC50 = 197 nM
CP0324941
5-[4-[1-[5-(1,3-thiazol-4-yl)-1,2,4-oxadiazol-3-yl]cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C19H16N6OS
 1
1 IC50 = 200 nM
CP0568937
(3S)-1-[3-[1-[4-(2-aminopyrimidin-5-yl)phenyl]cyclobutyl]-1,2,4-oxadiazol-5-yl]pyrrolidin-3-ol
   Show/Hide
C20H22N6O2
 1
1 IC50 = 202 nM
CP0367367
5-[4-[1-(5-pyridazin-4-yl-1,2,4-oxadiazol-3-yl)cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C20H17N7O
 1
1 IC50 = 240 nM
CP0566683
5-[4-[1-[5-[1-(2-aminoethyl)pyrazol-4-yl]-1,2,4-oxadiazol-3-yl]cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C21H22N8O
 1
1 IC50 = 240 nM
CP0508024
5-[4-[1-(5-pyridin-3-yl-1,2,4-oxadiazol-3-yl)cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C21H18N6O
 1
1 IC50 = 250 nM
CP0338909
5-[4-[1-[5-(1H-imidazol-5-yl)-1,2,4-oxadiazol-3-yl]cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C19H17N7O
 1
1 IC50 = 270 nM
CP0370072
US8575201, 15
   Show/Hide
C17H19N7O
 2
1 IC50 = 280 nM
2 IC50 = 2600 nM
CP0556268
5-[4-[1-[5-(1,3-oxazol-4-yl)-1,2,4-oxadiazol-3-yl]cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C19H16N6O2
 1
1 IC50 = 310 nM
CP0370070
1-[3-[1-[4-(2-aminopyrimidin-5-yl)phenyl]cyclobutyl]-1,2,4-oxadiazol-5-yl]azetidin-3-ol
   Show/Hide
C19H20N6O2
 1
1 IC50 = 315 nM
CP0408841
1-[3-[(1R)-1-[6-(2-aminopyrimidin-5-yl)pyridin-3-yl]-1-cyclopropylethyl]-1,2,4-oxadiazol-5-yl]piperidin-4-ol
   Show/Hide
C21H25N7O2
 1
1 IC50 = 324 nM
CP0324940
5-[4-[1-(5-pyrimidin-5-yl-1,2,4-oxadiazol-3-yl)cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C20H17N7O
 1
1 IC50 = 340 nM
CP0177303
5-[4-[(1S)-1-cyclopropyl-1-[5-(1-methylpyrazol-4-yl)-1,2,4-oxadiazol-3-yl]ethyl]phenyl]pyrimidin-2-amine
   Show/Hide
C21H21N7O
 1
1 IC50 = 350 nM
CP0324939
5-[4-[1-(5-pyrazin-2-yl-1,2,4-oxadiazol-3-yl)cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C20H17N7O
 1
1 IC50 = 360 nM
CP0326560
5-[4-[(2S)-3-methyl-2-[5-(1-methylpyrazol-4-yl)-1,2,4-oxadiazol-3-yl]butan-2-yl]phenyl]pyrimidin-2-amine
   Show/Hide
C21H23N7O
 1
1 IC50 = 360 nM
CP0082982
5-[4-[1-(5-piperidin-1-yl-1,2,4-oxadiazol-3-yl)cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C21H24N6O
 1
1 IC50 = 387 nM
CP0566684
5-[4-[1-(5-pyridazin-3-yl-1,2,4-oxadiazol-3-yl)cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C20H17N7O
 1
1 IC50 = 400 nM
CP0302587
3-[1-[4-(2-aminopyrimidin-5-yl)phenyl]cyclobutyl]-1,2,4-oxadiazol-5-amine
   Show/Hide
C16H16N6O
 1
1 IC50 = 440 nM
CP0326542
3-[1-[4-(2-aminopyrimidin-5-yl)phenyl]cyclobutyl]-N-ethyl-1,2,4-oxadiazol-5-amine
   Show/Hide
C18H20N6O
 1
1 IC50 = 460 nM
CP0568938
5-[4-[1-(5-pyrrolidin-1-yl-1,2,4-oxadiazol-3-yl)cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C20H22N6O
 1
1 IC50 = 467 nM
CP0335417
5-[4-[1-(5-phenyl-1,2,4-oxadiazol-3-yl)cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C22H19N5O
 1
1 IC50 = 470 nM
CP0110935
5-[4-[1-(5-piperazin-1-yl-1,2,4-oxadiazol-3-yl)cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C20H23N7O
 1
1 IC50 = 680 nM
CP0110071
3-[1-[4-(2-aminopyrimidin-5-yl)phenyl]cyclobutyl]-N,N-dimethyl-1,2,4-oxadiazol-5-amine
   Show/Hide
C18H20N6O
 1
1 IC50 = 690 nM
CP0177299
5-[4-[1-(5-pyrimidin-4-yl-1,2,4-oxadiazol-3-yl)cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C20H17N7O
 1
1 IC50 = 820 nM
CP0245532
2-[4-[3-[1-cyclopropyl-1-[4-[2-(ethylamino)pyrimidin-5-yl]phenyl]ethyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]-N,N-dimethylacetamide
   Show/Hide
C26H30N8O2
 1
1 IC50 = 1000 nM
CP0350126
5-[4-[3,3-dimethyl-1-[5-(1-methylpyrazol-4-yl)-1,2,4-oxadiazol-3-yl]cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C22H23N7O
 1
1 IC50 = 1500 nM
CP0556148
5-[4-[1-[5-(2H-triazol-4-yl)-1,2,4-oxadiazol-3-yl]cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C18H16N8O
 1
1 IC50 = 2100 nM
CP0514453
5-[4-[1-[5-(1-methylpyrazol-4-yl)-1,2,4-oxadiazol-3-yl]cyclopropyl]phenyl]pyrimidin-2-amine
   Show/Hide
C19H17N7O
 1
1 IC50 = 2200 nM
CP0283785
5-[4-[1-[5-(1H-1,2,4-triazol-5-yl)-1,2,4-oxadiazol-3-yl]cyclobutyl]phenyl]pyrimidin-2-amine
   Show/Hide
C18H16N8O
 1
1 IC50 = 2700 nM
CP0514450
5-[4-[(1S)-1-cyclobutyl-1-[5-(1-methylpyrazol-4-yl)-1,2,4-oxadiazol-3-yl]ethyl]phenyl]pyrimidin-2-amine
   Show/Hide
C22H23N7O
 1
1 IC50 = 3200 nM
CP0177300
3-[3-[1-[4-(2-aminopyrimidin-5-yl)phenyl]cyclobutyl]-1,2,4-oxadiazol-5-yl]-1H-pyridin-2-one
   Show/Hide
C21H18N6O2
 1
1 IC50 > 5000 nM
CP0177301
2-[4-[3-[1-[4-(2-aminopyrimidin-5-yl)phenyl]cyclobutyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]acetic acid
   Show/Hide
C21H19N7O3
 1
1 IC50 > 5000 nM
CP0508025
N-[3-[1-[4-(2-aminopyrimidin-5-yl)phenyl]cyclobutyl]-1,2,4-oxadiazol-5-yl]methanesulfonamide
   Show/Hide
C17H18N6O3S
 1
1 IC50 > 5000 nM
CP0519040
5-[4-[[5-(1-methylpyrazol-4-yl)-1,2,4-oxadiazol-3-yl]methyl]phenyl]pyrimidin-2-amine
   Show/Hide
C17H15N7O
 1
1 IC50 > 5000 nM
CP0350129
2-[4-[3-[(1R)-1-cyclopropyl-1-[4-[2-(propan-2-ylamino)pyrimidin-5-yl]phenyl]ethyl]-1,2,4-oxadiazol-5-yl]pyrazol-1-yl]-N,N-dimethylacetamide
   Show/Hide
C27H32N8O2
 1
1 IC50 > 50000 nM
Clinical Information about the Protein
Target 1 ( Arachidonate 5-lipoxygenase activating protein (FLAP) )
Target Type Discontinued Target
Disease 1 Target-related Disease  1
1 Asthma [ICD-11: CA23]
Discontinued Drug(s) 2 Discontinued Drugs  2
1 DG031 Discontinued in Phase 3
Asthma
2 GSK2190915 Discontinued in Phase 2
Asthma